Description

3-Methylfentanyl

3-Methylfentanyl is an opioid analgesic and is an analog of the potent opioid, fentanyl. 3-Methylfentanyl is one of the most powerful opioid drug sol illegall and is estimate to be between 400-6000 time more poten than morphine in certain case. 3-Methylfentanyl was initially discovere in 1974 and widespread illegal use of this drug has occurred since this time.

Pharmacodynamics

3-Methylfentanyl exhibit similar pharmacodynam effect to fentanyl but has been proven to be significant stronge in these effect due to increase bind affinity to the opioid receptor. Fentanyl, administered alone, has a strong affinity for opioid receptors. 3-methylfentanyl has the potential to be extremely hazardous when used without the prescription and supervision of a medical professional. Ingestion of this drug has resulted in numerous deaths among individuals using the drug recreationally.

Mechanism of action

Opiate receptor are couple with G-protein receptor and function as both positive and negative regulat of synaptic transmission via G-protein that activate effector protein. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitter such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibite. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Fentanyl’s analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.